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In vitro and in vivo effect of Eurycoma longifolia root extract on UDP-glucuronosyltransferase activity

Purwantiningsih Purwantiningsih,Abas Hj Hussin,Sabariah Ismail,Kit Lam Chan.




Abstract
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ABSTRACT

The aim of this research was to evaluate the effects of E. longifolia extract (ELE) on enzymes activity in the phase II drug metabolism on Sprague-Dawley (SD) rats especially on UGT activity, in-vivo and in-vitro. The UGT assay was performed based on method that Bock & Kohle described (2004). In the in-vivo study, the male SD rats were treated with ELE at doses ranging from 5 to 1000 mg/kg b.w. and 5, 25 and 50 mg/kg b.w for acute and sub-acute study, respectively. The ELE concentrations of 0.01 to 1000 µg/mL were used for in-vitro study. The pNP that consumed in the glucuronidation process reflected the UGT activity and was calculated using standard curve of pNP. UGT enzyme activity was inhibited significantly (P < 0.05) by ELE extract in the male rat for both acute and sub-acute experiments. ELE extract decreased the enzyme activity significantly (P < 0.05), at all concentrations tested in the in-vitro experiment when compared to the negative control group. ELE had a lower activity (the IC50 of 0.74 µg/mL) as compared to Na diclofenac (positive control) with an IC50 of 0.17 µg/mL. E. longifolia decreased the UGT enzyme activity significantly (P

Key words: Eurycoma longifolia, phase II drug metabolism, UGT enzyme activity






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